Pyrazole CCK1 receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free–Wilson additivity

https://doi.org/10.1016/j.bmcl.2005.09.041Get rights and content

Abstract

High-throughput screening revealed compound 1 as a potent antagonist of the CCK1 receptor. Here, we disclose the synthesis of combinatorial libraries by solid-phase synthesis on Kenner ‘safety catch’ resin. Additive QSAR models were used to determine a lack of consistent additive SAR within the matrix.

Section snippets

Acknowledgments

We thank Dale Boger for helpful discussions on the synthesis of compound 4, and Jiejun Wu and Heather McAllister for analytical support.

References and notes (6)

  • R. Herranz

    Med. Res. Rev.

    (2003)
    P. Tullio et al.

    Exp. Opin. Investig. Drugs

    (2000)
  • G. Varga

    Curr. Opin. Invest. Drugs

    (2002)
  • K. McClure et al.

    Bioorg. Med. Chem. Lett.

    (2005)
There are more references available in the full text version of this article.

Cited by (25)

  • Approaches using AI in medicinal chemistry

    2021, Computational and Data-Driven Chemistry Using Artificial Intelligence: Fundamentals, Methods and Applications
  • Use of Carbonyl Derivatives for Heterocyclic Synthesis

    2014, Comprehensive Organic Synthesis: Second Edition
View all citing articles on Scopus
View full text